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Bisindolylmaleimide V (CAS 113963-68-1)

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Application:
Bisindolylmaleimide V is a negative control for protein kinase C (PKC)-inhibitory activity
CAS Number:
113963-68-1
Purity:
≥98%
Molecular Weight:
341.3
Molecular Formula:
C21H15N3O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Bisindolylmaleimide V is used as a negative control for the PKC (protein kinase C)-inhibitory activity. Bisindolylmaleimide V, also known as BIM V, exhibits weak inhibition against protein kinase C (PKC) with an IC50 value exceeding 100 µM. Despite its limited potency as a PKC inhibitor, Bisindolylmaleimide V effectively impedes the activation of in vivo mitogen-stimulated protein kinase p70s6k/p85s6k (S6K) with an IC50 value of 8 µM. Functioning as a negative control for PKC inhibitors, Bisindolylmaleimide V serves as an inhibitor of S6K and a safeguard against necrosis. It stands as a cell-permeable compound, valuable for protein kinase C inhibition studies, showcasing an IC50 greater than 100 µM. Its capacity to halt the activation of p70s6k/p85s6k in vivo is demonstrated with an IC50 of 8 µM.


Bisindolylmaleimide V (CAS 113963-68-1) References

  1. The protein kinase C inhibitors bisindolylmaleimide I (GF 109203x) and IX (Ro 31-8220) are potent inhibitors of glycogen synthase kinase-3 activity.  |  Hers, I., et al. 1999. FEBS Lett. 460: 433-6. PMID: 10556511
  2. Protein kinase C activators inhibit the visual cascade in Limulus ventral photoreceptors at an early stage.  |  Dabdoub, A. and Payne, R. 1999. J Neurosci. 19: 10262-9. PMID: 10575023
  3. The effects of protein kinase C and calmodulin kinase II inhibitors on vestibular compensation in the guinea pig.  |  Sansom, AJ., et al. 2000. Brain Res. 882: 45-54. PMID: 11056183
  4. Involvement of protein kinase C in the presynaptic nicotinic modulation of [(3)H]-dopamine release from rat striatal synaptosomes.  |  Soliakov, L. and Wonnacott, S. 2001. Br J Pharmacol. 132: 785-91. PMID: 11159732
  5. Ro 31-6045, the inactive analogue of the protein kinase C inhibitor Ro 31-8220, blocks in vivo activation of p70(s6k)/p85(s6k): implications for the analysis of S6K signalling.  |  Marmy-Conus, N., et al. 2002. FEBS Lett. 519: 135-40. PMID: 12023032
  6. Inhibition of protein kinase C reduces ischemia-induced tyrosine phosphorylation of the N-methyl-d-aspartate receptor.  |  Cheung, HH., et al. 2003. J Neurochem. 86: 1441-9. PMID: 12950452
  7. Direct block by bisindolylmaleimide of the voltage-dependent K+ currents of rat mesenteric arterial smooth muscle.  |  Kim, A., et al. 2004. Eur J Pharmacol. 483: 117-26. PMID: 14729098
  8. Inhibitors of protein kinase C. 2. Substituted bisindolylmaleimides with improved potency and selectivity.  |  Davis, PD., et al. 1992. J Med Chem. 35: 994-1001. PMID: 1552513
  9. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.  |  Toullec, D., et al. 1991. J Biol Chem. 266: 15771-81. PMID: 1874734
  10. CCL2 is a negative regulator of AMP-activated protein kinase to sustain mTOR complex-1 activation, survivin expression, and cell survival in human prostate cancer PC3 cells.  |  Roca, H., et al. 2009. Neoplasia. 11: 1309-17. PMID: 20019839
  11. Production of interferon and of plaque enhancing factor by rinderpest-virus.  |  el-Zein, A. and Srour, E. 1985. Zentralbl Veterinarmed B. 32: 466-71. PMID: 2413658
  12. Inhibition of nicotinic responses of bovine adrenal chromaffin cells by the protein kinase C inhibitor, Ro 31-8220.  |  Marley, PD. and Thomson, KA. 1996. Br J Pharmacol. 119: 416-22. PMID: 8886429
  13. Muscarinic interactions of bisindolylmaleimide analogues.  |  Lazareno, S., et al. 1998. Eur J Pharmacol. 360: 281-4. PMID: 9851596

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Bisindolylmaleimide V, 1 mg

sc-202080
1 mg
$49.00

Bisindolylmaleimide V, 5 mg

sc-202080A
5 mg
$168.00